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首页> 外文期刊>Chemical and Pharmaceutical Bulletin >Multistep,Microwave Assisted,Solvent Free Synthesis and Antibacterial Activity of 6-Substituted-2,3,4-trihydropyrimido[1,2-c]9,10,11,12-tetrahydrobenzo[b]thieno[3,2-e]pyrimidines
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Multistep,Microwave Assisted,Solvent Free Synthesis and Antibacterial Activity of 6-Substituted-2,3,4-trihydropyrimido[1,2-c]9,10,11,12-tetrahydrobenzo[b]thieno[3,2-e]pyrimidines

机译:六取代的2,3,4-三氢嘧啶[1,2-c] 9,10,11,12-四氢苯并[b]噻吩并[3,2-e]的多步骤,微波辅助,无溶剂合成和抑菌活性嘧啶类

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摘要

A novel,efficient,microwave assisted route for the synthesis of 6-substituted-2,3,4-trihydropyrimido[l,2-c]-9,10,11,12-tetrahydrobenzo[b]thieno[3,2-e]pyrimidines in good yields has been developed.The intermediates,2-substituted-4-[3-hydroxy(propyl-1-amino)]5,6,7,8-tetrahydrobenzo[6]thieno[2,3-d|pyrimidines were obtained by irradiating 2-substituted-4-chloro-5,6,7,8-tetrahydrobenzo[6]thieno[2,3-d]pyrimidines with 1-amino-propanol under basic conditions in a microwave oven.4-Chlorothieno[2,3-d]pyrimidines were synthesized by microwave irradiation of equimolar mixture of 4-hydroxythieno[2,3-d]pyrimidines and phosphorus oxychloride.The final compounds were screened for antibacterial activity by Kirby Bauer's method using amicacin as the standard against various gram positive and gram negative bacteria.All the compounds showed antibacterial activity comparable with the standard.
机译:一种新颖,高效的微波辅助途径,用于合成6-取代的2,3,4-三氢嘧啶基[l,2-c] -9,10,11,12-四氢苯并[b]噻吩并[3,2-e已经开发了高产率的]嘧啶。中间体2-取代的-4- [3-羟基(丙基-1-氨基)] 5,6,7,8-四氢苯并[6]噻吩并[2,3-d |嘧啶是通过在碱性条件下,在微波炉中用1-氨基丙醇辐射2-取代的4-氯-5,6,7,8-四氢苯并[6]噻吩并[2,3-d]嘧啶来获得的。4-微波辐射4-羟基噻吩并[2,3-d]嘧啶和氯氧化磷的等摩尔混合物,合成了氯噻吩并[2,3-d]嘧啶。采用氨苄西林为标准,通过Kirby Bauer法筛选了最终化合物的抗菌活性。对各种革兰氏阳性和革兰氏阴性细菌均有效。所有化合物均显示出与标准品相当的抗菌活性。

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